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10.1016/j.bmcl.2015.03.012

http://scihub22266oqcxt.onion/10.1016/j.bmcl.2015.03.012
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C4567957!4567957!25813158
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suck abstract from ncbi


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pmid25813158      Bioorg+Med+Chem+Lett 2015 ; 25 (21): 4961-9
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  • Small cyclic agonists of iron regulatory hormone hepcidin #MMPMID25813158
  • Chua K; Fung E; Micewicz ED; Ganz T; Nemeth E; Ruchala P
  • Bioorg Med Chem Lett 2015[Nov]; 25 (21): 4961-9 PMID25813158show ga
  • Minihepcidins are in vitro and in vivo active mimetics of iron-regulatory hormone hepcidin. They contain various unusual amino acids including: N-substituted, ?-homo-, and D-amino acids with their combination depending on particular minihepcidin. In the current study, we sought to limit the use of unusual/more expensive amino acids derivatives by peptide cyclisation. Novel cyclic mimetics of hepcidin were synthesized and tested in vitro and showed activity at low nanomolar concentration. Nonetheless, the most active cyclic compound (mHS17) is approximately ten times less active than the parental minihepcidin PR73. Collectively, our findings suggest that cyclisation is viable approach in the synthesis of hepcidin mimetics.
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